Disease relevance of RH 5849

• On the other hand, RH-5849 showed no acute toxicity to tadpoles during the 96 h exposure even it was saturated in the test solutions [1].

High impact information on RH 5849

• RH 5849, a nonsteroidal ecdysone agonist: effects on a Drosophila cell line [2].
• Administration of the nonsteroidal ecdysteroid agonist RH-5849 (1,2-dibenzoyl-1-tert-butylhydrazine), but not 20-hydroxyecdysone, to tobacco hornworm (Manduca sexta) resulted in induction of midgut cytosolic ecdysone oxidase and ecdysteroid phosphotransferase activities [3].
• Induction of enzymes involved in molting hormone (ecdysteroid) inactivation by ecdysteroids and an agonist, 1,2-dibenzoyl-1-tert-butylhydrazine (RH-5849) [3].
• In addition, both 20-hydroxyecdysone and RH-5849 caused induction of ecdysteroid 26-hydroxylase activity in midgut mitochondria and microsomes, whereas 20-hydroxylase was induced to a lesser extent by 20-hydroxyecdysone in mitochondria and by either RH-5849 or 20-hydroxyecdysone in microsomes [3].
• Administration of the ecdysteroid agonist, RH-5849 (1,2-dibenzoyl, 1-tert-butyl hydrazone), or 20-hydroxyecdysone to the tobacco hornworm, Manduca sexta, results in induction of ecdysteroid 26-hydroxylase activity in midgut mitochondria and microsomes [4].

Chemical compound and disease context of RH 5849

• While in toxicity assays 20E was ineffective, most likely due to rapid metabolism, it was more potent than RH-5849 but less so than RH-5992 and RH-2485 in imaginal disc assays [5].
• We conclude that RH-5849 does not mimic makisterone-A, as is the case with ecdysone, and that toxicity is mediated instead through non-endocrine targets in this insect species [6].

Biological context of RH 5849

• Assessing the genotoxicity of imidacloprid and RH-5849 in human peripheral blood lymphocytes in vitro with comet assay and cytogenetic tests [7].
• For bilaterally applied RH-5849, the concentration needed for 50% block (IC50) was 79 +/- 6 microM (mean +/- SEM, n = 3), with a Hill coefficient near 2 [8].
• DNA damage scores increased with the exposure levels of both pesticides, and linear dose-effect relationships were observed for both imidacloprid (r2=0.98) and RH-5849 (r2=0.92) [7].
• In addition, RH-5849 halted the larval and pupal growth, where the untreated pupae were generally heavier than those produced from treated larvae [9].
• In regard to the fecundity and egg viability, RH-5849 induced a cessation of oviposition in females produced from 1-day-old and from 4-day-old larvae fed on diets treated with 160 and 200 ppm, respectively [9].

Anatomical context of RH 5849

• In vitro effect of nonsteroidal ecdysone agonist RH 5849 on fat body acid phosphatase activity in rice moth, Corcyra cephalonica (Insecta) [10].

Associations of RH 5849 with other chemical compounds

• Effect of bisacylhydrazine ecdysteroid mimics (RH-5849 and RH-5992) on chromosomal puffing, imaginal disc proliferation and pupariation in larvae of Drosophila melanogaster [11].
• Among the synthesized compounds, a 6-membered cyclic hydrazine bearing two benzoyl groups (5) exists in three conformational states in solution, and the major unsymmetrical conformer of 5 is similar to that of RH-5849 on the basis of 1H NMR and X-ray analyses [12].

Gene context of RH 5849

• The non-steroidal ecdysone agonist RH 5849 (1,2-dibenzoyl-1-tert-butylhydrazine) was found to inhibit in a dose-response and apparently competitive fashion the cytochrome P-450 dependent ecdysone 20-monooxygenase activity in the midgut of wandering stage last instar larvae of the tobacco hornworn, Manduca sexta [13].

Analytical, diagnostic and therapeutic context of RH 5849

• When RH-5849 was introduced inside the axon and internal perfusion was halted, IK increased within a few minutes to the control level, indicating that the compound diffused freely through the membrane and bound to a receptor within the plane of the membrane [8].

References